CA2703125C - Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer - Google Patents

Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer Download PDF

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Publication number
CA2703125C
CA2703125C CA2703125A CA2703125A CA2703125C CA 2703125 C CA2703125 C CA 2703125C CA 2703125 A CA2703125 A CA 2703125A CA 2703125 A CA2703125 A CA 2703125A CA 2703125 C CA2703125 C CA 2703125C
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CA
Canada
Prior art keywords
pyrazol
pyrrolo
6alkyl
pyrazin
independently selected
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA2703125A
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English (en)
French (fr)
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CA2703125A1 (en
Inventor
David J. Guerin
Joon Jung
Elizabeth Stanton
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Individual
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Merck Sharp and Dohme LLC
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Publication of CA2703125A1 publication Critical patent/CA2703125A1/en
Application granted granted Critical
Publication of CA2703125C publication Critical patent/CA2703125C/en
Expired - Fee Related legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2703125A 2007-10-25 2008-10-21 Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer Expired - Fee Related CA2703125C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34307P 2007-10-25 2007-10-25
US61/000,343 2007-10-25
PCT/US2008/011971 WO2009054941A1 (en) 2007-10-25 2008-10-21 Therapeutic compounds

Publications (2)

Publication Number Publication Date
CA2703125A1 CA2703125A1 (en) 2009-04-30
CA2703125C true CA2703125C (en) 2012-08-28

Family

ID=40579830

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2703125A Expired - Fee Related CA2703125C (en) 2007-10-25 2008-10-21 Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer

Country Status (6)

Country Link
US (1) US8183245B2 (enExample)
EP (1) EP2211620B1 (enExample)
JP (1) JP2011500806A (enExample)
AU (1) AU2008317406B2 (enExample)
CA (1) CA2703125C (enExample)
WO (1) WO2009054941A1 (enExample)

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US8877772B2 (en) 2008-11-25 2014-11-04 University Of Rochester Substituted pyrrolo[2,3-B]pyridines as MLK inhibitors
DE102009019962A1 (de) 2009-05-05 2010-11-11 Merck Patent Gmbh 3-([1,2,3]Triazol-4-yl)-pyrrolo[2,3-b]pyridinderivate
HRP20150701T1 (hr) * 2009-06-08 2015-08-28 Takeda Pharmaceutical Company Limited Spojevi dihidropirolonaftiridinona kao inhibitori jak
EP2338888A1 (en) * 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
WO2011137022A1 (en) * 2010-04-27 2011-11-03 Merck Sharp & Dohme Corp. Azaindoles as janus kinase inhibitors
WO2011149950A2 (en) 2010-05-24 2011-12-01 University Of Rochester Bicyclic heteroaryl kinase inhibitors and methods of use
WO2012054364A2 (en) * 2010-10-22 2012-04-26 Merck Sharp & Dohme Corp. Bicyclic diamines as janus kinase inhibitors
DE102010049877A1 (de) 2010-11-01 2012-05-03 Merck Patent Gmbh 7-((1,2,3)Triazol-4-yl)-pyrrolo(2,3) pyrazinderivate
CA2814826C (en) 2010-11-17 2019-02-12 Actelion Pharmaceuticals Ltd Bridged spiro[2.4]heptane ester derivatives
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
DE102010053347A1 (de) * 2010-12-03 2012-06-06 Merck Patent Gmbh 3-Hetaryl-substituierte Pyrrolo[2,3-b] pyridin-derivative als PDK1-Inhibitoren
DE102011008352A1 (de) 2011-01-12 2012-07-12 Merck Patent Gmbh 5-([1,2,3]Triazol-4-yl)-7H-pyrrolo-[2,3-d]pyrimidinderivate
DE102011009961A1 (de) 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
EP2688890B1 (en) 2011-03-22 2017-08-30 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
DE102011105469A1 (de) * 2011-06-24 2012-12-27 Merck Patent Gmbh 7-Azaindolderivate
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
DE102011119127A1 (de) 2011-11-22 2013-05-23 Merck Patent Gmbh 3-Cyanaryl-1H-pyrrolo[2.3-b]pyridin-Derivate
WO2013091539A1 (zh) * 2011-12-21 2013-06-27 江苏恒瑞医药股份有限公司 吡咯并六元杂芳环类衍生物、其制备方法及其在医药上的应用
SG11201408679XA (en) 2012-06-26 2015-01-29 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
US9593115B2 (en) 2012-09-21 2017-03-14 Advinus Therapeutics Ltd. Substituted fused tricyclic compounds, compositions, and medicinal applications thereof
DE102012019369A1 (de) 2012-10-02 2014-04-03 Merck Patent Gmbh 7-Azaindolderivat
WO2014085795A1 (en) 2012-11-30 2014-06-05 University Of Rochester Mixed lineage kinase inhibitors for hiv/aids therapies
US11491154B2 (en) 2013-04-08 2022-11-08 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
ES2921874T3 (es) 2014-02-28 2022-09-01 Nimbus Lakshmi Inc Inhibidores de TYK2 y usos de los mismos
ES2930585T3 (es) 2015-02-27 2022-12-19 Nimbus Lakshmi Inc Inhibidores de TYK2 y usos de los mismos
US10023571B2 (en) * 2015-09-02 2018-07-17 Nimbus Lakshimi, Inc. TYK2 inhibitors and uses thereof
CN109311896B (zh) 2016-06-30 2021-08-24 株式会社大熊制药 吡唑并嘧啶衍生物作为激酶抑制剂
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
JP6937828B2 (ja) 2016-11-23 2021-09-22 江蘇恒瑞医薬股▲ふん▼有限公司 ピロロ６員複素芳香環誘導体の製造方法、および中間体
WO2018134352A1 (en) * 2017-01-20 2018-07-26 Leo Pharma A/S Bicyclic amines as novel jak kinase inhibitors
IL277071B2 (en) 2018-03-08 2024-07-01 Incyte Corp AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS
AR117398A1 (es) 2018-03-12 2021-08-04 Abbvie Inc Inhibidores de la señalización mediada por tirosina cinasa 2
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
EP3947737A2 (en) 2019-04-02 2022-02-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
SG11202110714VA (en) * 2019-04-09 2021-10-28 Plexxikon Inc Condensed azines for ep300 or cbp modulation and indications therefor
WO2020212395A1 (en) 2019-04-16 2020-10-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
IL297437A (en) 2020-05-13 2022-12-01 Disc Medicine Inc Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
US20250283174A1 (en) 2022-05-16 2025-09-11 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation

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JP4787150B2 (ja) * 2003-03-06 2011-10-05 エーザイ・アール・アンド・ディー・マネジメント株式会社 Ｊｎｋ阻害剤
CA2560454C (en) * 2004-03-30 2013-05-21 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of jak and other protein kinases
US7361764B2 (en) * 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
WO2006015123A1 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
EP1828180A4 (en) 2004-12-08 2010-09-15 Glaxosmithkline Llc 1H-pyrrolo [2,3-BETA] PYRIDINE
US20060264442A1 (en) 2005-05-18 2006-11-23 Allergan, Inc. Methods for the treatment of ocular and neurodegenerative conditions in a mammal
DK2395004T3 (en) 2005-06-22 2016-03-21 Plexxikon Inc Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors
CA2615291A1 (en) * 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
DK3184526T3 (en) * 2005-12-13 2019-01-14 Incyte Holdings Corp PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR
WO2009054941A1 (en) * 2007-10-25 2009-04-30 Merck & Co., Inc. Therapeutic compounds

Also Published As

Publication number Publication date
CA2703125A1 (en) 2009-04-30
US20100210623A1 (en) 2010-08-19
EP2211620B1 (en) 2013-12-25
WO2009054941A1 (en) 2009-04-30
US8183245B2 (en) 2012-05-22
AU2008317406B2 (en) 2013-07-18
JP2011500806A (ja) 2011-01-06
EP2211620A4 (en) 2012-06-06
EP2211620A1 (en) 2010-08-04
AU2008317406A1 (en) 2009-04-30

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